Galnon

Chemical Name: 3-Cyclohexyl-N-(9H-fluoren-9-ylmethoxycarbonyl)-D,L-alanyl-D,L-lysine N-(4-methyl-2-oxo-2H-1-benzopyran-7-yl)amide
项目整合开发状态: Preclinical
项目研究机构: AstraZeneca (Originator)
合成路线:Coupling of N-alpha-Fmoc-N-epsilon-Boc-lysine (I) to 7-amino-4-methylcoumarin (II) by means of DCC produces the lysine amide (III).After acidic cleavage of the N-Boc protecting group of (III),the resultant primary amine (IV) is attached to chlorotrityl resin to produce (V).The Fmoc group of (V) is then removed with piperidine in DMF,yielding the lysinamide-bound resin (VI).Further coupling with N-Fmoc-cyclohexylalanine (VII) employing TBTU/HOAt furnishes the dipeptide amide resin (VIII).The title compound is finally cleaved from the solid support by means of trifluoroacetic acid in CH2Cl2.